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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
2421 Results for "
decrease
" in MedChemExpress (MCE) Product Catalog:
Products (2421)
2421 Results for "decrease" in MCE Product Catalog:
Cat. No.: HY-157125
CAS No.: 3026856-46-9
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
Cat. No.: HY-159978
CAS No.: 1628848-73-6
Synonyms: EOS789
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Atidafonat is an orally active sodium-dependent phosphate transporter inhibitor, with IC50 values of 6.8, 1.5, and 1.7 μM against human NaPi-IIb, PiT-1, PiT-2, respectively; and IC50 values of 3.9, 1.9, and 1.7 μM against rat NaPi-IIb, PiT-1, PiT-2, respectively. Atidafonat inhibits intestinal phosphate absorption, increases fecal phosphate excretion, reduces urinary phosphate excretion, and decreases the levels of serum phosphate, FGF23, and adult parathyroid hormone. Atidafonat ameliorates ectopic thoracic aortic calcification, renal injury and hyperphosphatemia, and inhibits the expression of fibrosis markers. Atidafonat can be used for the research of hyperphosphatemia and chronic kidney disease-mineral and bone disorder (CKD-MBD) .
Cat. No.: HY-160004
CAS No.: 1523493-53-9
Target:
PXL770 is an orally active, direct allosteric AMP-activated protein kinase (AMPK) activator. PXL770 decreases C26:0 levels, improves mitochondrial respiration, reduces expression of proinflammatory genes and induces expression of compensatory transporters (ABCD2/3) in ALD fibroblasts/lymphocytes. PXL770 normalizes plasma VLCFA levels, significantly reduces elevated VLCFA levels in brain and spinal cord in Abcd1 KO mice. PXL770 improves glycemia, dyslipidemia, and insulin resistance in ob/ob and high-fat diet (HFD)-fed mice. PXL770 can be used for the study of X-linked adrenoleukodystrophy (ALD), autosomal dominant polycystic kidney disease and nonalcoholic steatohepatitis (NASH) .
Cat. No.: HY-16638
CAS No.: 76849-19-9
Synonyms: PDDF
Target:
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CB 3717 is a potent inhibitor of human thymidylate synthetase, competitively binding with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10(-9) M). It also competitively inhibits human dihydrofolate reductase with dihydrofolate (Ki = 2.3 X 10(-8) M). In WI-L2 human lymphoblastoid cells, CB 3717 treatment led to a significant decrease in cellular dTTP levels and a notable increase in dUMP levels, indicating a disruption in nucleotide metabolism. The growth-inhibitory effect of CB 3717 was reversed by thymidine supplementation, demonstrating that thymidylate synthetase became rate-limiting in the presence of this compound. Delayed thymidine supplementation beyond 8 hours resulted in severe cytotoxicity, underscoring the critical timing of nucleotide rescue strategies in CB 3717-treated cells .
Cat. No.: HY-166478S
CAS No.: 1794817-24-5
Synonyms: Desmethylcarvedilol-d5; BM-14242-d5
Cat. No.: HY-16782A
CAS No.: 1416216-01-7
Synonyms: ARRY-614 hydrochloride
Research Areas:
Pexmetinib hydrochloride (ARRY-614 hydrochloride) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib hydrochloride binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib hydrochloride inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib hydrochloride can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis .
Cat. No.: HY-167856
CAS No.: 3034664-39-3
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RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
Cat. No.: HY-167856A
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RTI-122 dihydrochloride is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 dihydrochloride significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 dihydrochloride blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 dihydrochloride exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
Cat. No.: HY-168857
CAS No.: 3069913-37-4
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GSK-3β inhibitor 24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. GSK-3β inhibitor 24 increases GSK-3β phosphorylation at Ser9 site dose-dependently. GSK-3β inhibitor 24 inhibits the hyperphosphorylation of tau protein by decreasing the p-tau-Ser396 abundance. GSK-3β inhibitor 24 up-regulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2). GSK-3β inhibitor 24 demonstrates remarkable anti-Alzheimer's disease (AD) effects .
Cat. No.: HY-168895
CAS No.: 3125025-31-9
c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC50: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth .
Cat. No.: HY-171906
CAS No.: 65446-08-4
Synonyms: 1-Arachidonoyl-sn-glycerol 3-phosphate; 1-Arachidonoyl LPA; LPA (20:4)
Target:
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1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid containing arachidonic acid at the sn-1 position. It is a precursor to 1-arachidonoyl glycerol (1-Monoarachidin; HY-130567) . 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM . It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS . It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate .
Cat. No.: HY-173211
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anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic agent targeting mitochondrial DNA G4 (mtG4). Under white light irradiation, its IC50 against 4T1 cells is 0.42 μM. anti-TNBC agent-8 binds tightly to mtG4 and generates a large amount of reactive oxygen species (ROS) under white light irradiation, leading to the loss of mitochondrial membrane potential (MMP), a decrease in ATP production, and an increase in the ROS level. This, in turn, induces significant apoptosis in triple-negative breast cancer (TNBC) cells, exerting the activity of inhibiting tumor cell growth. anti-TNBC agent-8 can be used in the research of triple-negative breast cancer.
Cat. No.: HY-173388
CAS No.: 1019984-44-1
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TLR4-IN-2 (Compound Racemic-11k) is inhibitors of TLR4, JNK, and NF-κB. TLR4-IN-2 inhibits NO production in LPS-stimulated RAW264.7 cells with an IC50 value of 23.2 µM. TLR4-IN-2 exerts anti-inflammatory activity by inhibiting TLR4 expression, reducing JNK phosphorylation, thereby suppressing the activation of NF-κB, blocking the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and decreasing the production of inflammatory mediators such as NO, PGE 2, and TNF-α. TLR4-IN-2 is promising for research of inflammatory diseases, such as rheumatoid arthritis and various inflammatory disorders .
Cat. No.: HY-173408
CAS No.: 2899254-71-6
Target:
Nuclear Hormone Receptor 4A/NR4A Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase
Research Areas:
Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research .
Cat. No.: HY-17355AR
CAS No.: 104632-27-1
Synonyms: (R)-Pramipexole dihydrochloride (Standard); R-(+)-Pramipexole dihydrochloride (Standard); KNS-760704 dihydrochloride (Standard)
Target:
Reference Standards ATP Synthase Sodium Channel Glutathione Peroxidase NOD-like Receptor (NLR) Mitophagy Ferroptosis PINK1/Parkin Autophagy Apoptosis
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Dexpramipexole ((R)-Pramipexole) dihydrochloride (Standard) is the analytical standard of Dexpramipexole (dihydrochloride). This product is intended for research and analytical applications. Dexpramipexole dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
Cat. No.: HY-17355BS
CAS No.: 1432230-09-5
Synonyms: (R)-Pramipexole-d3 dihydrochloride; R-(+)-Pramipexole-d3 dihydrochloride; KNS-760704-d3 dihydrochloride
Cat. No.: HY-17357
CAS No.: 78281-72-8
Synonyms: AHR 9434; AL 6515
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Research Areas:
Neurological Disease Inflammation/Immunology Endocrinology Cancer
Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries .
Cat. No.: HY-174423
CAS No.: 1994348-72-9
Synonyms: NC-656
Iptriazopyrid is a 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor, with a Ki value of 24.3 nM against Arabidopsis thaliana and 33.3 nM against Oryza sativa. Iptriazopyrid binds to the active pocket of HPPD, occupies the catalytic site, inhibits carotenoid biosynthesis, prevents chloroplast formation, and induces albino and chlorotic symptoms in sensitive plants. Used as a herbicide, Iptriazopyrid can control barnyardgrass when applied alone, and its efficacy does not decrease when mixed with labeled residual herbicides. When Iptriazopyrid is mixed with 2,4-D or triclopyr, its barnyardgrass control effect shows an antagonistic effect. Iptriazopyrid is a triazole carboxamide herbicide that exhibits selectivity for Oryza sativa over Echinochloa crus-galli, and has partial tank-mix compatibility with synthetic auxin herbicides registered for rice .
Cat. No.: HY-174499
Cas9 Nickase D10A mRNA expresses a version of the Streptococcus pyogenes SF370 Cas9 protein (CRISPR Associated Protein 9) that contains a D10A amino acid substitution. This mRNA also contains a C-terminal nuclear localization signal followed by a HA tag.Cas9 functions as part of the CRISPR (clustered regularly interspaced short palindromic repeats) genome editing system. In the CRISPR system, an RNA guide sequence targets the site of interest and the Cas9 protein is employed to perform the DNA cleavage. While wild-type Cas9 creates a double-stranded break at the target site, Cas9 nickase creates a single-stranded break. This favors homology-directed repair and decreases the occurrence of non-homologous end joining.
Cat. No.: HY-175496
CAS No.: 2907705-12-6
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Acid Ceramidase-IN-3 is a acid ceramidase (aCDase) inhibitor. Acid Ceramidase-IN-3 inhibits the enzymatic activity of aCDase with a pIC 50 of 8.5 in enzymatic assays and 6.8 in A375 melanoma cellular assays. Acid Ceramidase-IN-3 promotes HSC inactivation, as measured by a dose-dependent
reduction in COL1A1 and ACTA2. Acid Ceramidase-IN-3 inhibits aCDase activity in HSCs, promotes HSC inactivation and suppresses YAP/TAZ nuclear localization. Acid Ceramidase-IN-3 increases Dynein/Kinesin (NDE1, NDEL1.
KIF3B, KIF15) while decreases several proteins involved with signaling pathway (SARM1, RGAP1,
PDGF-D,PDGFR-B). Acid Ceramidase-IN-3 can be used for the study of fibrotic diseases .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
